Free radical induced oxidation/reduction mechanisms of the hazardous water contaminant thiacloprid have been unravelled using pulse radiolysis techniques involving transient spectral analysis and redox titration experiments. The OH-induced oxidation of thiacloprid proceeds with appreciable rate,...

In order to examine the residues of thiacloprid (90 and 180 g a.i./ha) and deltamethrin (10 and 20 g a.i./ha) in fresh tea leaves, made tea and tea infusion, field experiments were conducted at three different locations viz. Kamalpur tea estate, Darjeeling; West Bengal, Teok tea Estate and AAU, ...

This work presents the characterization of novel synthesized WO3/Fe3O4 catalysts and investigates their photocatalytic activity for thiacloprid decomposition under UV and simulated sunlight radiation. Four WO3/Fe3O4 nanopowders with different amounts of WO3 were synthesized by chemical co-precip...

Biochars can significantly sorb pesticides, and reduce their bioavailability in agricultural soils. In this study, the effects of a type of biochar (BC500) on the sorption, degradation, bioaccumulation and bioavailability of thiacloprid, which is a commonly used insecticide, were investigated. T...

Possible genotoxic effect of thiacloprid on bovine cultures of whole blood was investigated using chromosomal aberrations (CAs), micronuclei (MN), sister chromatid exchanges (SCEs), DNA damage and apoptotic DNA fragmentation assays. The cells of whole blood were exposed to thiacloprid (30, 60, 1...

The cyano-substituted neonicotinoid insecticide, thiacloprid, is nowadays widely used in agriculture for controlling insect pests. However, it also simultaneously has adverse effects on the health of important pollinators, such as honey bees. Previous studies have reported that sublethal doses o...

Cu(OH)2 nanopesticides and organic insecticides are continuously applied to soil at a temporal interval, while knowledge about the impact of Cu(OH)2 nanopesticides on organic insecticides degradation is currently scarce, resulting in poorly comprehensive evaluation of the potential environmental...

The radical anions of 1-methyl-4-phenyl-5-nitrosoimidazole and 5-phenyl-4-nitrosoimidazole have been detected using temperature resolved e.s.r, spectroscopic techniques and are proposed as putative intermediates in the oxidation of thiols to disulphides by the nitrosoimidazoles.

1-Methyl-4-phenyl-5-nitrosoimidazole (5NO), which has properties consistent with the biologically active form of a 5-nitroimidazole, was radiolabeled (1-[14C]-methyl) and shown to bind to DNA, but at a rate too slow to account for its bactericidal effect. In the presence of physiological intrace...

Previously we have shown that some of 5-selenized salicylic acid derivatives exhibit glutathione peroxidase (GPx)-like activities higher than or equal to ebselen [Yu et al., Chem. Eur. J., 2008, 14, 7066; Org. Biomol. Chem., 2010, 8, 828]. For understanding the absence of GPx-like activity of th...

A series of novel nonphosphonate-based pTyr mimetics comprised (±)-3-(2-(2-fluorobenzyloxy)naphthalen-6-yl)-2-aminopropanoic acid derivatives were identified as reversible and competitive PTP1B inhibitors via a structure-based design approach. Among the compounds studied, 12h was found to have ...

Resistance to combretastatin A-4 is mediated by metabolic modification of the phenolic hydroxyl and ether groups of the 3-hydroxy-4-methoxyphenyl (B ring). Replacement of the B ring of combretastatin A-4 by a N-methyl-5-indolyl reduces tubulin polymerization inhibition (TPI) and cytotoxicity aga...

A series of forty two N-(1,3-diaryl-3-oxopropyl)amides were synthesized via an efficient, modified Dakin–West reaction and were evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Structure–activity relationship analyses have been presented. Selected active xanthine...

Unsymmetrical 3,5-disubstituted pyridylpiperazines were prepared from tribromopyridine in three coupling reactions. Key to the success of the syntheses is the palladium-catalyzed regioselective cross-coupling reaction in the 3-position of N-(3,5-dibromo-2-pyridyl)piperazines.

The first selective dopamine D4 agonist radioligand is described. The synthesis of these piperazine radioligands relied on the transformation of brominated precursors 4a and 4b with tritium gas in the presence of a sensitive cyano functional group. The specific activity of these two radioligands...

We herein describe the results of further evolution of glycogen synthase kinase (GSK)-3β inhibitors from our promising compounds containing a 3-methylmorpholine moiety. Transformation of the morpholine moiety into a piperazine moiety resulted in potent GSK-3β inhibitors. SAR studies focused on...

A strategy for the stereoselective preparation of enantiomerically enriched cis-2,6-disubstituted piperazines from amino acid precursors is described. The target compounds are generated in 95–99% ee with good to excellent levels of diastereoselectivity (usually 14:1 to >20:1) using Pd-catalyzed...

We have previously shown that 3-nitro-1H-1,2,4-triazole-based amines demonstrate significant trypanocidal activity, in particular against Trypanosoma cruzi, the causative parasite of Chagas disease. In the present work we further expanded our research by evaluating in vitro the trypanocidal acti...

A novel series of substituted piperazine-1-yl-pyrimidine derivatives were designed and synthesized as a new type of HIV-1 non-nucleoside inhibitors. Various N-substituted aromatic groups were incorporated into the piperazine ring through a simple and practical route to investigate the biological...

This account describes the convergent synthesis of (−)-okilactomycin. The first-generation approach focused on the assembly of two complex fragments through a Prins reaction of a dioxinone and α-hydroxy aldehyde. While this route was not ultimately successful, a related Maitland–Japp process e...